SU5416 is also a potent competitive inhibitor of KIT (the receptor for stem cell factor) and less potently the PDGF receptor (indirectly involved in angiogenesis), but is not directly cytotoxic by itself (Antonian et al, 2000; Smolich et al, 2001; Yee et al, 2002).
Horie, M. et al. NB-598: a potent competitive inhibitor of squalene epoxidase.
More companies are learning to exploit patents as potent competitive weapons and as a source of unexpected revenues.
These derivatives are potent, competitive, and reversible inhibitors of PTP1B with improved caco-2 permeability.
2-Methyleneglutarate, closely resembling iminoglutarate, was a potent competitive inhibitor of the glutamate dehydrogenase reaction.
TMC-95's natural cyclic tripeptide metabolites represent potent competitive proteasome inhibitors.
Enzymatic kinetic screening revealed that compound 7 was a potent competitive inhibitor of human O-GlcNAcase (Ki = 185.6 μM).
Bromination also enhances inhibition, and 3,5-dibromokynurenine is a potent competitive inhibitor with a KI value of 1.5 μM.
Alberts, A. W. et al. Mevinolin, a highly potent competitive inhibitor of hydroxylmethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent.
Several galactonoamidines were previously identified as very potent competitive inhibitors that exhibit stabilizing hydrophobic interactions of the aglycon in the active site of β-galactosidase (Aspergillus oryzae).
"Offshoring has created a truly global operating model for financial services, unleashing a new and potent competitive dynamic that is changing the rules of the game for the entire industry," the report said.
